2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. AZD6538

AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain.

For research use only. We do not sell to patients.

AZD6538 Chemical Structure

AZD6538 Chemical Structure

CAS No. : 453566-30-8

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AZD6538 Related Antibodies

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Description

AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain[1].

IC50 & Target

rat mGluR5

3.2 ± 0.1 nM (IC50)

human mGluR5

13.4 ± 1.3 nM (IC50)

In Vitro

AZD6538 completely reverses the glutamate-stimulated (EC80, 80 μM) phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with an IC50 of 51 ± 3 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZD6538 Related Antibodies
Molecular Weight

291.24

Formula

C15H6FN5O
CAS No.
Appearance

Solid

SMILES

N#CC1=CC=C(N=C1)C2=NOC(C3=CC(F)=CC(C#N)=C3)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 4 mg/mL (13.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4336 mL 17.1680 mL 34.3359 mL
5 mM 0.6867 mL 3.4336 mL 6.8672 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4336 mL 17.1680 mL 34.3359 mL 85.8399 mL
5 mM 0.6867 mL 3.4336 mL 6.8672 mL 17.1680 mL
10 mM 0.3434 mL 1.7168 mL 3.4336 mL 8.5840 mL
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AZD6538 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD6538453566-30-8AZD 6538AZD-6538mGluRMetabotropic glutamate receptorsbrain penetrantneuropathic painphosphatidyl inositolInhibitorinhibitorinhibit

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